MCC-555
(Synonyms: Isaglitazone,Netoglitazone,RWJ 241947) 目录号 : GC14595A structural homolog of rosiglitazone
Cas No.:161600-01-7
Sample solution is provided at 25 µL, 10mM.
MCC-555, also known as RWJ-241947, is a novel peroxisome proliferator–activated receptor γ ligand [1].
The PPARγ receptors mainly express in adipose tissue, colon and macrophages involved in regulating fatty acid storage and glucose metabolism. It has been identified that PPARγ is the major functional receptor for the thiazolidinedione class of insulin-sensitizing drugs. The PPARγ receptor is implicated in the processes of adipogenesis and systemic insulin action [2].
MCC-555 (5 μmol/L) exhibited an apoptotic activity in human colorectal cancer cells. MCC-555 significantly increased NAG-1 expression in a PPARγ-independent manner. In HCT-116 cells, treatment with MCC-555 induced apoptosis. MCC-555 affected NAG-1 mRNA stability. MCC-555 treatment induced rapid phosphorylation of ERK1/2 [1]. In various solid and hematological tumor cell lines, MCC-555 showed antiproliferative activity against prostate cancer cells, with the strongest effect against the androgen-independent PC-3 prostate cancer cells [2].
In male beige/nude/X-linked immunodeficient (BNX) mice, treatment with MCC-555 profoundly suppressed growth of PC-3 prostate cancer xenografts with prominent apoptosis, fibrosis, and inflammatory and giant cell reaction. The experimented mice showed significantly decreased cholesterol [3].
References:
[1] Yamaguchi K, Lee S H, Eling T E, et al. A novel peroxisome proliferator–activated receptor γ ligand, MCC-555, induces apoptosis via posttranscriptional regulation of NAG-1 in colorectal cancer cells[J]. Molecular cancer therapeutics, 2006, 5(5): 1352-1361.
[2] Spiegelman B M. PPAR-gamma: adipogenic regulator and thiazolidinedione receptor[J]. Diabetes, 1998, 47(4): 507-514.
[3] Kumagai T, Ikezoe T, Gui D, et al. RWJ-241947 (MCC-555), a unique peroxisome proliferator-activated receptor-γ ligand with antitumor activity against human prostate cancer in vitro and in beige/nude/X-linked immunodeficient mice and enhancement of apoptosis in myeloma cells induced by arsenic trioxide[J]. Clinical Cancer Research, 2004, 10(4): 1508-1520.
Cas No. | 161600-01-7 | SDF | |
别名 | Isaglitazone,Netoglitazone,RWJ 241947 | ||
化学名 | 5-[[6-[(2-fluorophenyl)methoxy]-2-naphthalenyl]methyl]-2,4-thiazolidinedione | ||
Canonical SMILES | FC1=CC=CC=C1COC2=CC(C=CC(CC3SC(NC3=O)=O)=C4)=C4C=C2 | ||
分子式 | C21H16FNO3S | 分子量 | 381.4 |
溶解度 | ≤1mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide | 储存条件 | Store at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
||
Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.6219 mL | 13.1096 mL | 26.2192 mL |
5 mM | 0.5244 mL | 2.6219 mL | 5.2438 mL |
10 mM | 0.2622 mL | 1.311 mL | 2.6219 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet